Orally rapidly disintegrating tablet that contains two or more types of particles

Abstract

The present invention provides an orally rapidly-disintegrating tablet comprising at least two particles. Regarding medicaments with unpleasant taste, the present invention provides a tablet comprising such medicament having a suitable hardness so that the tablet can be handled without any difficulty in the period from the formulation of the tablet to the administration thereof (in particular, a tablet which can maintain the hardness thereof when it is stored under a humidified condition); a small size; no unpleasant taste; a pleasant feeling in a mouth after administration; and an excellent disintegration character in the oral cavity and an excellent dissolution character in the gastrointestinal tract.

The invention claimed is: 
     
       1. An orally rapidly-disintegrating tablet comprising the following particles (1) and (2):
 (1) a medicament-containing particle comprising the following ingredients (a) to (c):
 (a) a medicament 
 (b) a water-soluble polymer, and 
 (c) a sugar or sugar alcohol, 
 
 
       wherein all of the ingredients (a) to (c) are granulated and then particulated, and
 (2) a spray-dried particle comprising the following ingredients (d) to (f):
 (d) mannitol, or mannitol and xylitol 
 (e) carboxymethylcellulose, and 
 (f) a disintegrant, 
 
 
       wherein all of the ingredients (d) to (f) are dispersed in a solvent for dispersion and then spray-dried. 
     
     
       2. The orally rapidly-disintegrating tablet of  claim 1 , wherein the water-soluble polymer (b) is at least one compound selected from the group consisting of polyvinylpyrrolidone, methylcellulose, pullulan, polyvinyl alcohol, hydroxypropyl methylcellulose, and hydroxypropyl cellulose. 
     
     
       3. The orally rapidly-disintegrating tablet of  claim 2 , wherein the water-soluble polymer (b) is at least one compound selected from the group consisting of methylcellulose, pullulan, polyvinyl alcohol, and hydroxypropyl cellulose. 
     
     
       4. The orally rapidly-disintegrating tablet of  claim 1 , wherein the sugar or sugar alcohol (c) is at least one compound selected from the group consisting of mannitol, xylitol, lactose, erythritol, trehalose, sucrose, maltitol, and lactitol. 
     
     
       5. The orally rapidly-disintegrating tablet of  claim 4 , wherein the sugar or sugar alcohol (c) is at least one compound selected from the group consisting of mannitol, xylitol, lactose, erythritol, and lactitol. 
     
     
       6. The orally rapidly-disintegrating tablet of  claim 1 , wherein the disintegrant (f) is at least one compound selected from the group consisting of a low-substituted hydroxypropyl cellulose, croscarmellose sodium, microcrystalline cellulose, carmellose calcium, hydroxypropyl starch, and rice starch. 
     
     
       7. The orally rapidly-disintegrating tablet of  claim 6 , wherein the disintegrant (f) is a low-substituted hydroxypropyl cellulose. 
     
     
       8. The orally rapidly-disintegrating tablet of  claim 1 , wherein the spray-dried particle (2) further comprises ingredient (g):
 (g) an inorganic compound, 
 
       and all of the ingredients (d) to (g) are dispersed in the solvent for dispersion and then spray-dried. 
     
     
       9. The orally rapidly-disintegrating tablet of  claim 8 , wherein the inorganic compound (g) is at least one compound selected from the group consisting of magnesium aluminometasilicate, magnesium aluminosilicate, anhydrous silicic acid, light anhydrous silicic acid, calcium silicate, and dibasic calcium phosphate. 
     
     
       10. The orally rapidly-disintegrating tablet of  claim 1 , wherein each content of:
 (a) the medicament is 1 wt % to 30 wt %, 
 (b) the water-soluble polymer is 3 wt % to 45 wt %, and 
 (c) the sugar or sugar alcohol is 40 wt % to 90 wt %, 
 
       per 100 wt % of the whole weight of the medicament-containing particle (1). 
     
     
       11. The orally rapidly-disintegrating tablet of  claim 1 , wherein each content of:
 (d) the mannitol, or mannitol and xylitol is 65 wt % to 95 wt %, 
 (e) the carboxymethylcellulose is 1 wt % to 20 wt %, and 
 (f) the disintegrant is 1 wt % to 20 wt %, 
 
       per 100 wt % of the whole weight of the spray-dried particle (2). 
     
     
       12. The orally rapidly-disintegrating tablet of  claim 11 , wherein the spray-dried particle (2) further comprises:
 (g) an inorganic compound in an amount of 0.01 wt % to 15 wt %, 
 
       per 100 wt % of the whole weight of the spray-dried particle (2). 
     
     
       13. The orally rapidly-disintegrating tablet of  claim 1 , wherein the medicament (a) is 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]-methyl]benzamide. 
     
     
       14. The orally rapidly-disintegrating tablet of  claim 1 , wherein each content of:
 the medicament-containing particle (1) is 5 wt % to 37 wt %, and 
 the spray-dried particle (2) is 15 wt % to 90 wt %, 
 
       per 100 wt % of the whole weight of the orally rapidly-disintegrating tablet.